Axitinib/Axitinib Medication Guidelines

1. Overview of Drugs

Common name: Axitinib (Axitinib)

Business name: Inlyta (Inlyta)

Alias: axitinib

2. Indications

Axitinib is mainly used to treat the following diseases:

1) First-line advanced renal cell carcinoma (RCC): It can be used in combination with avelumab or pembrolizumab and is suitable for first-line treatment of patients with advanced renal cell carcinoma.

2) Second-line advanced renal cell carcinoma: As monotherapy for patients with advanced renal cell carcinoma after failure of previous systemic therapy.

3. Usage and dosage

1) Recommended dosage:

First-line treatment in combination with avelumab: The initial dose is 5 mg orally twice daily 12 hours apart. May be used in combination with avelumab 800 mg as an intravenous infusion every two weeks until disease progression or unacceptable toxicity. Consider increasing the dose of axitinib if necessary.

First-line treatment with pembrolizumab: Initial dose is 5 mg orally twice daily 12 hours apart. May be used in combination with pembrolizumab 200 mg every 3 weeks or 400 mg every 6 weeks as an intravenous infusion over 30 minutes until disease progression or unacceptable side effects. Also consider increasing the dose of axitinib when clinically necessary.

Second-line treatment: When used as a single agent, the recommended starting oral dose is 5 mg twice daily, with or without food, approximately 12 hours apart.

2) Medication instructions: Patients are advised to swallow the entire tablet with a full glass of water. In the event of vomiting or missed doses, patients should not take the missed dose but should continue taking it at the next prescribed time.

3) Dose adjustment: The dose should be adjusted according to the patient’s safety and tolerability. During treatment, if the patient tolerates axitinib for two consecutive weeks without grade 2 or above adverse reactions, has normal blood pressure, and does not use antihypertensive drugs, an increase may be considered.

4. Adverse reactions

In clinical studies, common adverse reactions of axitinib include:

Diarrhea

high blood pressure

fatigue

difficulty speaking

nausea and vomiting

Loss of appetite

weight loss

Palm-Plantar Paresthesia Syndrome

hemorrhage

hypothyroidism

Increased proteinuria

Cough and constipation

In addition, serious adverse events related to arteries, including aneurysms and dissections, have been reported post-marketing.

5. Supply and storage

Axitinib tablet specifications include1mg and 5mg. Storage conditions are 20°C to 25°C (68°F to 77°F), with permitted temperature deviations from 15°C to 30°C (59°F to 86°F).

6. Mechanism of action

Axitinib works by inhibiting receptor tyrosine kinases, specifically vascular endothelial growth factor receptors (VEGFR)-1, -2, and -3. These receptors are closely related to pathological angiogenesis, tumor growth, and cancer progression. Studies have shown that axitinib can inhibit VEGF-mediated endothelial cell proliferation and survival, and shows the effect of inhibiting tumor growth and VEGFR-2 phosphorylation in mouse models.

Reference materials:https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=84137882-e000-47da-bd5b-fa76ab3c76f9##